de Klerk J M, van het Schip A D, Zonnenberg B A, van Dijk A, Quirijnen J M, Blijham G H, van Rijk P P
Department of Nuclear Medicine, University Hospital Utrecht, The Netherlands.
J Nucl Med. 1996 Feb;37(2):244-9.
Rhenium-186-1,1-hydroxyethylidene diphosphonate (186Re-HEDP) has been used for the palliative treatment of metastatic bone pain. A Phase 1 dosage escalation study was performed using 186Re-HEDP in patients with metastatic breast cancer.
Twelve patients with metastatic breast cancer were studied. Each patient had at least four bone metastases and adequate hematological function. Groups of three consecutive patients were treated with dosages starting at 1295 MBq (35 mCi) and increasing to 2960 MBq (80 mCi) (escalated in increments of 555 MBq).
A transient increase in pain ("flare" reaction) was observed in six patients. Two patients who received 2960 MBq 186Re-HEDP showed Grades 3 (platelets 25-50 x 10(9)/l) and 4 (platelets < 25 x 10(9)/l) platelet toxicity, which was defined as unacceptable. Prior to treatment, alkaline phosphatase levels were elevated in seven cases. These patients showed a transient decline in alkaline phosphatase levels during the first 4 wk.
The maximum tolerated administered activity of 186Re-HEDP in patients with metastatic breast cancer is 2405 MBq (65 mCi). Thrombocytopenia proved to be the dose-limiting toxicity, which could not be predicted adequately by the administered activity. Changes of alkaline phosphatase levels suggest anti-tumor effects of 186Re-HEDP.
铼 - 186 - 1,1 - 羟基亚乙基二膦酸盐（186Re - HEDP）已用于转移性骨痛的姑息治疗。对转移性乳腺癌患者进行了一项使用186Re - HEDP的1期剂量递增研究。
对12例转移性乳腺癌患者进行了研究。每位患者至少有四处骨转移且血液学功能良好。连续三组患者接受的剂量从1295 MBq（35 mCi）开始，逐渐增加至2960 MBq（80 mCi）（以555 MBq的增量递增）。
6例患者出现疼痛短暂增加（“闪烁”反应）。两名接受2960 MBq 186Re - HEDP的患者出现3级（血小板25 - 50×10⁹/L）和4级（血小板<25×10⁹/L）血小板毒性，这被定义为不可接受。治疗前，7例患者碱性磷酸酶水平升高。这些患者在最初4周内碱性磷酸酶水平出现短暂下降。
转移性乳腺癌患者中186Re - HEDP的最大耐受给药活度为2405 MBq（65 mCi）。血小板减少被证明是剂量限制毒性，给药活度无法充分预测。碱性磷酸酶水平的变化提示186Re - HEDP具有抗肿瘤作用。
